CAS: 312636-16-1; 4-((4-(4-Chlorophenyl)Thiazol-2-yl)Amino)Phenol

上下游产品

4-(4-(4-chlorophenyl)thiazol-2-ylamino)phenol hydrobromide sodium thi°Cyanide 4-amino-phenol 4-chlorobenzoylmethyl bromide

N-苯甲酰基-N'-(4-羟基苯基)硫脲置于sodium Hydroxide体系中,用 乙醇,水 作为反应溶剂,化学反应 1.5H,反应生成 4-[[4-(4-氯苯基)-2-噻唑基]氨基]苯酚
参考文献:Multi-Dimensional Target Profiling Of N,4-Diaryl-1,3-Thiazole-2-Amines As Potent Inhibitors Of Eicosanoid Metabolism
标题:Multi-Dimensional Target Profiling Of N,4-Diaryl-1,3-Thiazole-2-Amines As Potent Inhibitors Of Eicosanoid Metabolism
摘要:Eicosanoids Like Leukotrienes And Prostaglandins Play A Considerable Role In Inflammation. Produced Within The Arachidonic Acid (Aa) Cascade,These Lipid Mediators Are Involved In The Pathogenesis Of Pain As Well As Acute And Chronic Inflammatory Diseases Like Rheumatoid Arthritis And Asthma. With Regard To The Lipid Cross-Talk Within The Aa Pathway,A Promising Approach For An Effective Anti-Inflammatory Therapy Is The Development Of Inhibitors Targeting More Than One Enzyme Of This Cascade. Within This Study,Thirty N-4-Diaryl-1,3-Thiazole-2-Amine Based Compounds With Different Substitution Patterns Were Synthesized And Tested In Various Cell-Based Assays To Investigate Their Activity And Selectivity Profile Concerning Five Key Enzymes Involved In Eicosanoid Metabolism (5-,12-,15-Lipoxygenase (Lo),Cyclooxygenase-1 And-2 (Cox-1/-2)). With Compound 7,2-(4-Phenyl)Thiazol-2-Ylamino)Phenol (St-1355),A Multi-Target Ligand Targeting All Tested Enzymes Is Presented,Whereas Compound 9,2-(4-(4-Chlorophenyl)Thiazol-2-Ylamino)Phenol (St-1705),Represents A Potent And Selective 5-Lo And Cox-2 Inhibitor With An Ic50 Value Of 0.9 +/-0.2 μm (5-Lo) And A Residual Activity Of 9.1 +/-1.1% At 10 μm (Cox-2 Product Formation). The Promising Characteristics And The Additional Non-Cytotoxic Profile Of Both Compounds Reveal New Lead Structures For The Treatment Of Eicosanoid-Mediated Diseases.
DOI:10.1016/j.Ejmech.2014.07.025

专利信息

专利号:US-9687477-B2
优先权日:2011-06-01
标 题 :Modulation of sphingosine 1-phosphate metabolizing enzymes for the treatment of negative-strand RNA virus infections
发明人：HAHM BUMSUK; SEO YOUNG-JIN; ALEXANDER STEPHEN; MADHUVANTHI VIJAYAN
权利人:HAHM BUMSUK; SEO YOUNG-JIN; ALEXANDER STEPHEN; MADHUVANTHI VIJAYAN; UNIV MISSOURI
摘要:The present invention relates to compounds and methods for the prevention or treatment of infections by negative strand RNA viruses, such as influenza virus and measles virus, wherein said compounds delay or inhibit viral replication by modulating the level or activity of a polypeptide involved in the synthesis or degradation of sphingosine-1-phosphate (S1P) in a cell, tissue, or subject. The methods involve administration of one or more compounds which modulate the level of gene expression, where the gene encodes a polypeptide involved in regulating the metabolic level of S1P, or modulate the level or activity of a polypeptide involved in regulating the metabolic level of S1P, such as sphingosine kinase (SK) and S1P lyase (SPL). Exemplary methods are directed towards reducing the level of SW by reducing the level or activity of one or more SKs, increasing the level or activity of one or more SPLs, or a combination of both steps.